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Nafamostat mesilate (FUT-175) Serine Protease inhibitor

Name: Nafamostat mesilate (FUT-175)
Brand: Selleck Chemicals
SKU: S1386
Rating: 5 (20 reviews)

Cat. No.: S1386

Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor used as an anticoagulant during hemodialysis. It blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. This compound also attenuates inflammation and apoptosis.

Nafamostat mesilate (FUT-175) Serine Protease inhibitor Chemical Structure

Estructura química

Peso molecular: 539.58

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Control de calidad (Quality Control)

Lote: Pureza: 99.81%

99.81

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Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Tiempo de incubación	Descripción de la actividad	PMID
NS0	Function assay	15 mins	Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay, IC50=0.005μM.	29701962
Sf9	Function assay	30 mins	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells using Boc-QLR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay, Ki=0.025μM.	25882520
Sf9	Function assay	30 mins	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry, IC50=0.15μM.	25882520
MDA-MB-231	Function assay	15 mins	Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting, EC50=0.49μM.	25408834
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	539.58	Fórmula	C₁₉H₁₇N₅O₂.2CH₄O₃S	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	82956-11-4	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (185.32 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 100 mg/mL

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	serine protease
In vitro	Nafamostat mesilate (FUT-175) significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. It prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. This compound completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. It inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC). Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM. It produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM.
In vivo	Nafamostat mesilate (FUT-175) (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. It (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). This compound (10 mg/kg) suppresses tryptase activity in the mouse skin. It inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. When combined with Gemcitabine, it improves the body weight loss of mice induced by Gemicitabine.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/8713783/ [2] https://pubmed.ncbi.nlm.nih.gov/8029816/ [3] https://pubmed.ncbi.nlm.nih.gov/17826743/ [4] https://pubmed.ncbi.nlm.nih.gov/16359660/ [5] https://pubmed.ncbi.nlm.nih.gov/19661331/ [6] https://pubmed.ncbi.nlm.nih.gov/32312781/ [7] https://pubmed.ncbi.nlm.nih.gov/35974017/

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